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1. 发明授权

US4866176A 8-Piperazinyl-1,7-naphthyridine derivative having pharmaceutical activity 失效
标题翻译：具有药物活性的8-哌嗪基-1,7-萘啶衍生物
公开(公告)号：US4866176A
公开(公告)日：1989-09-12
申请号：US84836
申请日：1987-08-13
申请人： Haruyoshi Honda , Yuko Yoshida , Tadayuki Kouda , Hideaki Matsuda , Tatsuhiko Katori
发明人： Haruyoshi Honda , Yuko Yoshida , Tadayuki Kouda , Hideaki Matsuda , Tatsuhiko Katori
IPC分类号： A61K31/495 , A61P9/04 , A61P9/06 , A61P25/04 , A61P29/00 , C07D471/04
CPC分类号： C07D471/04
摘要： A 8-piperazinyl-1,7-naphthyridine derivative represented by the following formula (I): ##STR1## in which R represents a hydrogen atom, formyl group, acyl group, aroyl group, heteroaroyl group, substituted phenyl group, pyridyl group, aralkyl group or substituted or unsubstituted benzenesulfonyl group; and an acid adduct salt thereof. The compound has excellent antiinflammatory, antiarrhythmic and cardiotonic effects, and thus is useful as an antiinflammatory drug and a medicine for circulatory organs.

2. 发明授权

US5710152A Benzoazine derivative or salt thereof and pharmaceutical compostion comprising the same 失效
标题翻译：苯并嗪衍生物或其盐和包含其的药物组合物
公开(公告)号：US5710152A
公开(公告)日：1998-01-20
申请号：US791269
申请日：1997-01-30
申请人： Yoshihiro Nagao , Yoshikuni Ito , Jiro Kotake , Tadayuki Kouda , Haruyoshi Honda , Susumu Sato , Hideaki Matsuda
发明人： Yoshihiro Nagao , Yoshikuni Ito , Jiro Kotake , Tadayuki Kouda , Haruyoshi Honda , Susumu Sato , Hideaki Matsuda
IPC分类号： C07D417/12 , A61K31/505 , A61K31/535 , A61K31/54
CPC分类号： C07D417/12
摘要： A benzoazine derivative represented by the following formula (1), ##STR1## wherein R.sup.1 represents an alkyl group, alkoxy group, halogen atom, halogenoalkyl group, amino group, hydroxy group, benzyloxy group which may have a substituent, cyano group, carbamoyl group, acyl group, nitro group, carboxy group, or sulfonamide group; R.sup.2 and R.sup.3 may be the same or different and each individually represents a hydrogen atom or an alkyl group, or R.sup.2 and R.sup.3 indicate in combination an alkylene group having 2-7 carbon atoms; R.sup.4 and R.sup.5 may be the same or different and each individually represents a hydrogen atom or an alkyl group; X denotes O, S, or N--R.sup.6 (wherein R.sup.6 represents a hydrogen atom, an alkyl group, or an aryl group or pyridyl group which may have a substituent); m is an integer from 0 to 4; and n is an integer from 1 to 3, or a salt of the benzoazine derivative. The compound exhibits superior effects for reducing blood glucose value, plasma insulin value, and plasma triglyceride value, and is useful as a medicament for preventing or treating diabetes, hyperlipidemia, and obesity.
摘要翻译：由下式（1）表示的苯并嗪衍生物，其中R1表示烷基，烷氧基，卤素原子，卤代烷基，氨基，羟基，可具有取代基的苄氧基，氰基，氨基甲酰基，酰基，硝基，羧基或磺酰胺基; R2和R3可以相同或不同，各自独立地表示氢原子或烷基，或R2和R3组合表示具有2-7个碳原子的亚烷基; R 4和R 5可以相同或不同，各自独立地表示氢原子或烷基; X表示O，S或N-R6（其中R6表示氢原子，烷基或可具有取代基的芳基或吡啶基）; m为0〜4的整数; n为1〜3的整数，或苯并嗪衍生物的盐。该化合物对于降低血糖值，血浆胰岛素值和血浆甘油三酯值具有优异的效果，并且可用作预防或治疗糖尿病，高脂血症和肥胖症的药物。

3. 发明授权

US4728659A Aminomethyl derivatives and preparation process thereof as well as platelet aggregation inhibitors containing same 失效
标题翻译：氨基甲基衍生物及其制备方法以及含有它的血小板聚集抑制剂
公开(公告)号：US4728659A
公开(公告)日：1988-03-01
申请号：US748686
申请日：1985-06-25
申请人： Susumu Sato , Tadayuki Kouda , Tatsuhiko Katori
发明人： Susumu Sato , Tadayuki Kouda , Tatsuhiko Katori
IPC分类号： C07D213/80 , A61K31/455
CPC分类号： C07D213/80
摘要： Disclosed herein are aminomethyl derivatives each of which is of the following general formula (I): ##STR1## wherein A represents a group --C.tbd.C-- or --CH.dbd.CH--, Y represents a group ##STR2## (in which R.sub.3 being a lower alkyl or alkoxy group or a halogen atom) or ##STR3## (in which R.sub.4 being a hydrogen atom or R.sub.3), and R.sub.1 and R.sub.2 represent individually a lower alkyl group, with a proviso that Y is other than the group ##STR4## when A means the group --CH.dbd.CH--, their preparation process and platelet aggregation inhibitors containing same.
摘要翻译：本文公开了氨基甲基衍生物，其各自具有以下通式（I）：其中A表示基团-C3B-或-CH = CH-，Y表示基团（在其中R3为低级烷基或烷氧基或卤素原子）或（其中R4为氢原子或R3），R1和R2分别表示低级烷基，条件是Y不为组，当A表示基团-CH = CH-时，其制备方法和含有该组的血小板聚集抑制剂。

4. 发明授权

US4588822A Physiologically active substances SS 12538, their preparation and a novel microorganism producing same 失效
标题翻译：生理活性物质SS 12538，它们的制备和生产相同的新型微生物
公开(公告)号：US4588822A
公开(公告)日：1986-05-13
申请号：US482409
申请日：1983-04-06
申请人： Junji Oono , Kenichi Yano , Junichi Sato , Tadayuki Kouda , Yoichiro Ogawa , Kouichi Yokoi , Toshiaki Nakashima
发明人： Junji Oono , Kenichi Yano , Junichi Sato , Tadayuki Kouda , Yoichiro Ogawa , Kouichi Yokoi , Toshiaki Nakashima
IPC分类号： C07D309/38 , C12P17/06 , C07D309/32
CPC分类号： C12R1/465 , C07D309/38 , C12P17/06 , Y10S435/886
摘要： Disclosed are novel physiologically active substance SS 12538, process for its preparation and a novel microorganism producing the same.The novel physiologically active substance SS 12538 is represented by the following formula (I): ##STR1## in which R represents a hydrogen atom, a methyl group or an ethyl group. SS 12538 is obtained by inoculating a novel strain S 12538 in a nutrient-containing medium and cultivating aerobically.SS 12538 has excellent vasodilating action and antibiotic action against a certain gram positive bacteria and dermatophytes.
摘要翻译：公开了新型生理活性物质SS 12538，其制备方法和生产该生物活性物质的新型微生物。新型生理活性物质SS 12538由下式（I）表示：其中R表示氢原子，甲基或乙基的式（I）化合物。通过将新菌株S 12538接种在含营养培养基中并有氧培养获得SS 12538。 SS 12538对某些革兰氏阳性菌和皮肤癣菌具有优异的血管扩张作用和抗生素作用。

5. 发明授权

US4450109A Thiazinobenzimidazole derivatives 失效
标题翻译：噻嗪基苯并咪唑衍生物
公开(公告)号：US4450109A
公开(公告)日：1984-05-22
申请号：US417596
申请日：1982-09-13
申请人： Hiromichi Eto , Teruo Kohmoto , Tadayuki Kouda , Youichiro Ogawa , Susumu Sato , Tadayuki Kuraishi , Toshiaki Nakashima
发明人： Hiromichi Eto , Teruo Kohmoto , Tadayuki Kouda , Youichiro Ogawa , Susumu Sato , Tadayuki Kuraishi , Toshiaki Nakashima
IPC分类号： A61K31/54 , A61K31/55 , A61P9/08 , A61P9/10 , A61P9/12 , C07D513/04
CPC分类号： C07D513/04
摘要： The specification describes novel thiazinobenzimidazole derivatives represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2 and X represent a wide variety of substituent groups respectively. The above thiazinobenzimidazole derivatives may be prepared by reacting corresponding 2-hydroxymethyl thiazinobenzimidazole derivatives with corresponding reactive derivatives of carboxylic acid or halogenide or by reacting 2-p-toluenesulfonyloxymethyl-thiazinobenzimidazole derivatives with sodium azides, thiols, phenols or amines. The above thiazinobenzimidazole derivatives wherein X is OH may be prepared by reducing their corresponding 2-alkoxycarbonyl derivatives. Where X represents a p-toluenesulfonyloxy group, the thiazinobenzimidazole derivatives may be obtained by reacting corresponding 2-hydroxymethyl-thiazinobenzimidazole derivatives with p-toluenesulfonyl chloride. Where X stands for an N-substituted 2-(homo)piperazinomethyl group, 2-(homo)piperazinomethyl-thiazinobenzimidazole derivatives are reacted with reactive compounds to introduce the desired substituent groups. The thiazinobenzimidazole derivatives according to this invention are useful as medicament for circulatory systems.
摘要翻译：该说明书描述了由以下通式表示的新型噻唑并苯并咪唑衍生物：其中R1，R2和X分别代表多种取代基。上述噻唑并苯并咪唑衍生物可以通过使相应的2-羟甲基噻嗪基苯并咪唑衍生物与羧酸或卤化物的相应反应性衍生物反应或通过2-对甲苯磺酰氧甲基 - 噻嗪基苯并咪唑衍生物与叠氮化钠，硫醇，酚或胺的反应来制备。其中X是OH的上述噻嗪基苯并咪唑衍生物可以通过还原它们相应的2-烷氧基羰基衍生物来制备。当X代表对甲苯磺酰氧基时，噻吩并苯并咪唑衍生物可以通过相应的2-羟甲基 - 噻嗪基苯并咪唑衍生物与对甲苯磺酰氯反应而得到。其中X代表N-取代的2-（均）哌嗪基甲基，2-（高）哌嗪基甲基 - 噻嗪基苯并咪唑衍生物与反应性化合物反应以引入所需的取代基。根据本发明的噻嗪基苯并咪唑衍生物可用作循环系统的药物。

6. 发明授权

US4369309A Thiazinobenzimidazole derivatives 失效
标题翻译：噻嗪基苯并咪唑衍生物
公开(公告)号：US4369309A
公开(公告)日：1983-01-18
申请号：US240219
申请日：1981-03-03
申请人： Hiromichi Eto , Teruo Kohmoto , Tadayuki Kouda , Youichiro Ogawa , Susumu Sato , Tadayuki Kuraishi , Toshiaki Nakashima
发明人： Hiromichi Eto , Teruo Kohmoto , Tadayuki Kouda , Youichiro Ogawa , Susumu Sato , Tadayuki Kuraishi , Toshiaki Nakashima
IPC分类号： A61K31/54 , A61K31/55 , A61P9/08 , A61P9/10 , A61P9/12 , C07D513/04 , C09B23/10 , C07D417/14
CPC分类号： C07D513/04
摘要： The specification describes novel thiazinobenzmidazole derivatives represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2 and X represent a wide variety of substituent groups respectively. The above thiazinobenzimidazole derivatives may be prepared by reacting corresponding 2-hydroxymethyl thiazinobenzimidazole derivatives with corresponding reactive derivatives of carbonylic acid or halogenide or by reacting 2-p-toluenesulfonyloxymethyl-thiazinobenzimidazole derivatives with sodium azides, thiols, phenols or amines. The above thiazinobenzimidazole derivatives wherein X in OH may be prepared by reducing their corresponding 2-alkoxycarbonyl derivatives. Where X represents a p-toluenesulfonyloxy group, the thiazinobenzimidazole derivatives may be obtained by reacting corresponding 2-hydroxymethyl-thiazinobenzimidazole derivatives with p-toluenesulfonyl chloride. Where X stands for an N-substituted 2-(homo)piperazinomethyl group, 2-(homo)piperazinomethyl-thiazinobenzimidazole derivatives are reacted with reactive compounds to introduce the desired substituent groups. The thiazinobenzimidazole derivatives according to this invention are useful as medicament for circulatory systems.
摘要翻译：该说明书描述了由以下通式表示的新型噻嗪并咪唑衍生物：其中R1，R2和X分别代表各种各样的取代基。上述噻唑并苯并咪唑衍生物可以通过使相应的2-羟甲基噻嗪基苯并咪唑衍生物与羰基酸或卤化物的相应反应性衍生物反应，或通过2-对甲苯磺酰氧基甲基 - 噻嗪基苯并咪唑衍生物与叠氮化钠，硫醇，酚或胺反应来制备。其中X中的X可以通过还原其相应的2-烷氧基羰基衍生物来制备上述噻唑并苯并咪唑衍生物。当X代表对甲苯磺酰氧基时，噻吩并苯并咪唑衍生物可以通过相应的2-羟甲基 - 噻嗪基苯并咪唑衍生物与对甲苯磺酰氯反应而得到。其中X代表N-取代的2-（均）哌嗪基甲基，2-（高）哌嗪基甲基 - 噻嗪基苯并咪唑衍生物与反应性化合物反应以引入所需的取代基。根据本发明的噻嗪基苯并咪唑衍生物可用作循环系统的药物。

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